Clematis Radix, Trichosanthis Radix, and Prunellae Spica are well known for medicinal plants. Each medicinal plant has long been used for the treatment of general inflammations, such as various swellings, wounds, bronchitis, mastitis, tonsillitis, and anal fistula and also for the relief of various symptoms such as cold or numb hands, painful knees, painful waist and shoulder, feeble in health and pain in the skin, in the form of aqueous plant extract. These symptoms are similar to general arthritis including chronic rheumatism in terms of the modern pathological concept.
Clematis Radix, a root of Clematis mandshurica and the same genera in plant taxonomy, is distributed in the shady forest throughout Asia. It is collected in autumn, washed cleanly after removing cormophyte and root hair, chopped finely and dried in the sun to be used as a medicinal use. Clematis Radix, a non-toxic medicinal plant, has long been used for the treatment of the following symptoms: pains in the extremities; motor disturbance in knee joints; and paralysis in the extremities. In particular, Clematis Radix has been frequently used as a miraculous drug in those patients who feel uncomfortable while standing due to the coldness in waist, knees and feet. It is well known that Clematis Radix has various constituents of flavanone glycosides such as clematin, etc. and saponins such as clemontanoside A, clemontanoside B, clemontanoside C, and clemontanoside S, glucoses, and sterols [Research Archives of Useful Plants Resources in Korea, Korea Research Institute of Chemical Technology, pp 780-781 (1988), 2. An Explanatory Diagram of Korean Medicinal plants, Youngrim Pub., pp 489-490 (1990)].
Trichosanthis Radix, known as “multifarious medicine” or “Karokon”, is a non-toxic medicinal herb prepared by collecting roots of Trichosnathes kirilowii and the same genera in plant taxonomy, which are perennial liana plants, in autumn. The outer shells of cleanly washed roots are removed and the rest of the roots are cut appropriately and dried in the sun for medicinal use. Trichosanthis Radix has been widely used for excretion of pus, vanishing the boil, detoxification and antipyretic effect and also effective for diseases symptomized by thirst, various swellings, mastitis, and anal fistula. It has been investigated up to now that Trichosanthis Radix contains trichosanthin as proteins, arginine and citruline as amino acids, and palmitic acid and linoleic acid as fatty acids. Recently Trichosanthis Radix is found to contain bryonolic acid, 4-hydroxybenzoic acid, α-spinastero as sterols [Research Archives of Useful Plants Resources in Korea, Korea Research Institute of Chemical Technology, pp 354-357 (1988), 2. An Explanatory Diagram of Korean Medicinal Plants, Youngrim Pub., pp 960-963 (1990)].
Prunellae Spica, a flower or upper part of Prunella vulgaris and the same genera in plant taxonomy, is a non-toxic medicinal herb prepared by collecting the flower, when it is half withered during summer, and drying in the sun. Prunellae Spica has been widely used for the treatment of the following symptoms: chronic swellings, smallpox, acute mastitis and lymphatic tuberculosis. Prunellae Spica is also effective in the destructing lumps (generated in a lower stomach owing to extravasated blood) or others, while treating beriberi and numbness in the extremities. It has been reported that Prunellae Spica contains saponins such as oleanolic acid glycosides and ursolic acid glycosides, etc, and also contains carotene, vitamin C, vitamin K, tannin, caffeic acid and chlorogenic acid. Rosmarinic acid is also found in Prunellae Spica [Research Archives of Useful Plant Resources in Korea, Korea Research institute of Chemical Technology, pp 480-482 (1988); Chemical Research for Prunellae Spica, Lee Jak-pyung et al., Bulletin of Medical College in Beijing, 17(4), pp 297-299 (1985); Pharm. Acta. Helv., 66, No. 7, pp 185-188 (1991)].
The conventional oriental herbal books (e.g., Dong-Eui-Bo-gam, Hyangyak Gibsung-bang and Kwangjee Beakub) or related literatures refer to the medical efficacy of herbs and processes of manufacturing aqueous herbal solutions. However, they only described a single prescription of each of these medicinal plants but not a formulation available for the manufacture of aqueous herbal solution from appropriate combinations of sorted medicinal plants by harvest place and harvest time to control the content of active ingredients. Furthermore, these medicinal plants were prepared by hot water extraction method, and any substances extracted by above method showed no acquisition of detailed knowledge on biologically active ingredients.
On the other hand, the inventors of the present invention have disclosed a process of extraction and purified biologically effective ingredients from an extract of Clematis Radix, Trichosanthis Radix, and Prunellae Spica in a certain ratio, being useful for alleviating acute/chronic inflammation; for inhibiting platelet and whole blood aggregation, enzyme activities associated with degradation of joint tissue, abnormally proliferated immunocytes, and inflammation-inducing enzymes; for scavenging activity of toxic active oxygen radical; and further for the treatment of chronic rheumatoid arthritis (U.S. Pat. No. 5,910,307). U.S. Pat. No. 5,910,307 is characterized by mixing Clematis Radix, Trichosanthis Radix, and Prunellae Spica in a weight ratio of 1:0.5-2:0.5-1.5 and extracting the mixture with water or aqueous alcoholic solution; partitioning with water-saturated n-butanol and concentrating the alcohol layer under reduced pressure; and concentrating the result with water under constant boiling and lyophilizing to obtain an extract in powder form.
In the continuous study, the inventors have realized that it is difficult to standardize the extracts of Clematis Radix, Trichosanthis Radix, and Prunellae Spica with simple weight ratio since the content variation of each ingredient significantly varies with harvest place and harvest time. This further makes it difficult to merchandize such combined extracts since it is hard to obtain the reproducibility of active ingredients having analgesic and anti-inflammatory effects, blood circulation enhancing effect, arthritis therapeutic effect and cartilage protection. Thereupon, the inventors have made an extensive research to maximize the pharmacological efficiency of herbal drug composition with the reproducibility. As a result, we have developed a method to optimize the efficiency of cartilage protection effect as well as the analgesic and anti-inflammatory effect, blood circulation enhancing effect, and arthritis therapeutic effect by controlling the content of rosmarinic acid in the herbal drug composition, not the extract weight ratio of Clematis Radix, Trichosanthis Radix, and Prunellae Spica. In addition, it was possible to merchandize medicinal herbs with the reproducibility.
The present invention, an improved invention of U.S. Pat. No. 5,910,307, provides significant improvement in merchandizing by optimizing the herbal extract composition of Clematis Radix, Trichosanthis Radix, and Prunellae Spica with the proper content of rosmarinic acid, maximizes pharmacological efficiencies over the conventional herbal composition and further provides novel therapeutic effects.